HUP9902017A2 - Aminosav- és hidroxisav-származékokkal szubsztituált benzamidinszármazékok és antikoagulánsokként történő alkalmazásuk - Google Patents

Aminosav- és hidroxisav-származékokkal szubsztituált benzamidinszármazékok és antikoagulánsokként történő alkalmazásuk

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Publication number
HUP9902017A2
HUP9902017A2 HU9902017A HUP9902017A HUP9902017A2 HU P9902017 A2 HUP9902017 A2 HU P9902017A2 HU 9902017 A HU9902017 A HU 9902017A HU P9902017 A HUP9902017 A HU P9902017A HU P9902017 A2 HUP9902017 A2 HU P9902017A2
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Hungary
Prior art keywords
alkyl
derivatives
halogen
hydrogen
atom
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HU9902017A
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English (en)
Inventor
Monica Kochanny
Raju Mohan
Michael M. Morrissey
Howard P. Ng
Weija Yun
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Berlex Laboratories, Inc.
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Publication date
Application filed by Berlex Laboratories, Inc. filed Critical Berlex Laboratories, Inc.
Publication of HUP9902017A2 publication Critical patent/HUP9902017A2/hu
Publication of HUP9902017A3 publication Critical patent/HUP9902017A3/hu
Publication of HU223604B1 publication Critical patent/HU223604B1/hu

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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/62—Oxygen or sulfur atoms
    • C07D213/63—One oxygen atom
    • C07D213/64—One oxygen atom attached in position 2 or 6
    • C07D213/643—2-Phenoxypyridines; Derivatives thereof
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/62—Oxygen or sulfur atoms
    • C07D213/69—Two or more oxygen atoms
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
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    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/62—Oxygen or sulfur atoms
    • C07D213/70—Sulfur atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/72—Nitrogen atoms
    • C07D213/74—Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D251/00—Heterocyclic compounds containing 1,3,5-triazine rings
    • C07D251/02—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings
    • C07D251/12—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D251/14—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hydrogen or carbon atoms directly attached to at least one ring carbon atom
    • C07D251/16—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hydrogen or carbon atoms directly attached to at least one ring carbon atom to only one ring carbon atom
    • C07D251/18—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hydrogen or carbon atoms directly attached to at least one ring carbon atom to only one ring carbon atom with nitrogen atoms directly attached to the two other ring carbon atoms, e.g. guanamines
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D251/00—Heterocyclic compounds containing 1,3,5-triazine rings
    • C07D251/02—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings
    • C07D251/12—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D251/14—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hydrogen or carbon atoms directly attached to at least one ring carbon atom
    • C07D251/16—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hydrogen or carbon atoms directly attached to at least one ring carbon atom to only one ring carbon atom
    • C07D251/20—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hydrogen or carbon atoms directly attached to at least one ring carbon atom to only one ring carbon atom with no nitrogen atoms directly attached to a ring carbon atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D251/00—Heterocyclic compounds containing 1,3,5-triazine rings
    • C07D251/02—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings
    • C07D251/12—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D251/26—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with only hetero atoms directly attached to ring carbon atoms
    • C07D251/30—Only oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D251/00—Heterocyclic compounds containing 1,3,5-triazine rings
    • C07D251/02—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings
    • C07D251/12—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D251/26—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with only hetero atoms directly attached to ring carbon atoms
    • C07D251/38—Sulfur atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D251/00—Heterocyclic compounds containing 1,3,5-triazine rings
    • C07D251/02—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings
    • C07D251/12—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D251/26—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with only hetero atoms directly attached to ring carbon atoms
    • C07D251/40—Nitrogen atoms
    • C07D251/48—Two nitrogen atoms

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Abstract

A találmány a Xa-faktőr enzimet gátló hatással rendelkező, és ígyantikőagűlánsőkként felhasználható (I), (II), (III), (IV), (V), (VI)vagy (VII) általánős képletű vegyületekre, - amelyek képletében A -C(R8)= csőpőrt vagy nitrőgénatőm; Z1 és Z2 őxigén-, kénatőm, -N(R13)- vagy -OCH2- csőpőrt; R1 és R4 hidrőgén-, halőgénatőm, alkil-, nitrő-, -OR13, -C(O)OR13, -C(O)N(R13)R14, -N(R13)R14, -N(R13)C(O)R13, -N(H)S(O)2R16 csőpőrt; R2 amidinő-, -C(NH)N(H)OR13, -C(NH)N(HC(O)OR16, -C(NH)N(H)C(O)R13, -C(NH)N(H)S(O)2R16, -C(NH)N(H)C(O)N(H)R13 csőpőrt; R3 halőgénatőm, alkil-, halőgén-alkil-, nitrő-, aminő-, űreidő-,gűanidinő-, -OR13, amidinő-, -C(NH)N(H)OR13, -C(O)N(R13)R14, -R15-C(O)N(R13)R14, -CH(OH)C(O)N(R13)R14, -N(R13)R14, -R15-N(R13)R14, -C(O)OR13, -R15-C(O)OR13, -N(R13)C(O)R13, adőtt esetben alkilcsőpőrttalszűbsztitűált (1,2)-tetrahidrő-pirimidinil-, (1,2)-imidazőlil- vagy(1,2)-imidazőlinilcsőpőrt; R5 és R6 hidrőgén-, halőgénatőm, alkil-, halőgén-alkil-, nitrő-, -N(R13)R14, -C(O)OR13, -C(O)N(R13)R14, -C(O)N(R13)CH2C(O)N(R13)R14, -N(R13)C(O)N(R13)R14, -N(R13)C(O)R14, -N(R13)S(O)2R16, -N(R13)C(O)N(R13)CH2C(O)N(R13)R14 csőpőrt; R7 -N(R9)-[C(R10)(R11)]n-R12 csőpőrt (n 1, 2, 3 vagy 4), vagy -O-[C(R10)(R11)]n-R12 csőpőrt (n 1, 2, 3, 4, 5 vagy 6); R8 hidrőgén-, halőgénatőm, alkilcsőpőrt - és gyógyászatilagelfőgadható sóikra, a vegyületeket tartalmazó gyógyszerkészítményekre,valamint a gyógyszerkészítmény előállítási eljárására vőnatkőzik. ŕ
HU9902017A 1996-02-12 1997-02-07 Aminosav- és hidroxisavszármazékokkal szubsztituált benzamidinszármazékok és antikoagulánsokként történő alkalmazásuk HU223604B1 (hu)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US08/599,834 US5994375A (en) 1996-02-12 1996-02-12 Benzamidine derivatives substituted by amino acid and hydroxy acid derivatives and their use as anti-coagulants
PCT/IB1997/000098 WO1997029067A1 (en) 1996-02-12 1997-02-07 Benzamidine derivatives substituted by amino acid and hydroxy acid derivatives and their use as anti-coagulants

Publications (3)

Publication Number Publication Date
HUP9902017A2 true HUP9902017A2 (hu) 1999-09-28
HUP9902017A3 HUP9902017A3 (en) 2000-06-28
HU223604B1 HU223604B1 (hu) 2004-10-28

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Application Number Title Priority Date Filing Date
HU9902017A HU223604B1 (hu) 1996-02-12 1997-02-07 Aminosav- és hidroxisavszármazékokkal szubsztituált benzamidinszármazékok és antikoagulánsokként történő alkalmazásuk

Country Status (23)

Country Link
US (4) US5994375A (hu)
EP (1) EP0888271B1 (hu)
JP (1) JP3762790B2 (hu)
KR (1) KR19990082480A (hu)
CN (1) CN1211232A (hu)
AT (1) ATE265409T1 (hu)
AU (1) AU715992B2 (hu)
CA (1) CA2245925A1 (hu)
CZ (1) CZ255098A3 (hu)
DE (1) DE69728869T2 (hu)
DK (1) DK0888271T3 (hu)
ES (1) ES2221032T3 (hu)
HU (1) HU223604B1 (hu)
IL (1) IL125285A (hu)
NO (1) NO312834B1 (hu)
NZ (1) NZ326452A (hu)
PL (1) PL186474B1 (hu)
PT (1) PT888271E (hu)
RU (1) RU98117078A (hu)
SK (1) SK283306B6 (hu)
UA (1) UA51694C2 (hu)
WO (1) WO1997029067A1 (hu)
ZA (1) ZA971183B (hu)

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NO983671D0 (no) 1998-08-11
CZ255098A3 (cs) 1999-01-13
SK283306B6 (sk) 2003-05-02
IL125285A (en) 2002-11-10
UA51694C2 (uk) 2002-12-16
ZA971183B (en) 1997-09-18
SK109298A3 (en) 1999-02-11
CN1211232A (zh) 1999-03-17
PT888271E (pt) 2004-09-30
ATE265409T1 (de) 2004-05-15
JP2000505431A (ja) 2000-05-09
ES2221032T3 (es) 2004-12-16
HUP9902017A3 (en) 2000-06-28
PL328412A1 (en) 1999-01-18
DE69728869D1 (de) 2004-06-03
DK0888271T3 (da) 2004-08-16
RU98117078A (ru) 2000-06-10
US6242454B1 (en) 2001-06-05
AU715992B2 (en) 2000-02-17
AU1454897A (en) 1997-08-28
PL186474B1 (pl) 2004-01-30
US5994375A (en) 1999-11-30
CA2245925A1 (en) 1997-08-14
US6071912A (en) 2000-06-06
IL125285A0 (en) 1999-03-12
EP0888271B1 (en) 2004-04-28
HU223604B1 (hu) 2004-10-28
NZ326452A (en) 2000-02-28
US6166088A (en) 2000-12-26
EP0888271A1 (en) 1999-01-07
KR19990082480A (ko) 1999-11-25
NO312834B1 (no) 2002-07-08
NO983671L (no) 1998-09-11
DE69728869T2 (de) 2005-01-05
WO1997029067A1 (en) 1997-08-14
JP3762790B2 (ja) 2006-04-05
EP0888271A4 (en) 2000-03-15

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